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Kinase Inhibitor
No.168(January 2016)
Tyrphostins are small molecules which are designed to bind to the substrate subsite of the protein tyrosine kinase (PTK) domain.1) Tyrphostin A1 (1) inhibits STAT4 phosphorylation.2) STAT3 phosphorylation is also down-regulated by 1.2) On the other hand, because of acting epidermal growth factor receptor kinase (EGFRK) with a high IC50 ( >1,250 μM) ,1) 1 is sometimes used as a negative control.3,4)
1 has been used for enhancement of rAAV (recombinant adeno-associated virus) mediated transgene expression.5) The research article shows that, when the cells were treated at 500 μM of 1, a 1,000-fold enhancement was achieved up to 100 virus articles per cell level.5)
STAT: signal transducer and activator of transcription
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References
- 1)Tyrphostins I: Synthesis and biological activity of rotein tyrosine kinase inhibitors
- 2)Differential requirements for JAK2 and TYK2 in T cell proliferation and IFN-γ production induced by IL-12 alone or together with IL-18
- 3)Constitutive activation of a slowly migrating isoform of Stat3 in mycosis fungoides: Tyrphostin AG490 inhibits Stat3 activation and growth of mycosis fungoides tumor cell lines
- 4)Epidermal growth factor system regulates mucin production in airways
- 5)Enhancement of recombinant adeno-associated virus type 2-mediated transgene expression in a lung epithelial cell line by inhibition of the epidermal growth factor receptor
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